Title of article
Ircinialactams: Subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae Original Research Article
Author/Authors
Walter Balansa، نويسنده , , Robiul Islam، نويسنده , , Frank Fontaine، نويسنده , , Andrew M. Piggott، نويسنده , , Hua Zhang، نويسنده , , Timothy I. Webb، نويسنده , , Daniel F. Gilbert، نويسنده , , Joseph W. Lynch، نويسنده , , Robert J. Capon، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2010
Pages
8
From page
2912
To page
2919
Abstract
Screening an extract library of >2500 southern Australian and Antarctic marine invertebrates and algae for modulators of glycine receptor (GlyR) chloride channels identified three Irciniidae sponges that yielded new examples of a rare class of glycinyl lactam sesterterpene, ircinialactam A, 8-hydroxyircinialactam A, 8-hydroxyircinialactam B, ircinialactam C, ent-ircinialactam C and ircinialactam D. Structure–activity relationship (SAR) investigations revealed a new pharmacophore with potent and subunit selective modulatory properties against α1 and α3 GlyR isoforms. Such GlyR modulators have potential application as pharmacological tools, and as leads for the development of GlyR targeting therapeutics to treat chronic inflammatory pain, epilepsy, spasticity and hyperekplexia.
Keywords
marine natural products , Glycine receptor (GlyR) chloride channels , Glycinyl lactam sesterterpenes , Irciniidae
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2010
Journal title
Bioorganic and Medicinal Chemistry
Record number
1307295
Link To Document